Biological Pathway: Reactome:R-HSA-9669936

Sorafenib-resistant KIT mutants related metabolites

find 2 related metabolites which is associated with the biological pathway Sorafenib-resistant KIT mutants

this pathway object is a organism specific pathway, which is related to taxonomy Homo sapiens (human).

Sorafenib is a type II tyrosine kinase inhibitor that is approved for use in hepatocellular and renal cell carcinoma. It is active against KIT receptors with mutations in the ATP-binding cleft and the activation loop, with the exception of substitutions at D816, which are resistant (Guida et al, 2007; Heinrich et al, 2012; Serrano et al, 2019; Weisberg et al, 2019; reviewed in Roskoski, 2018; Klug et al, 2012).

Sorafenib

4-(4-(3-(4-Chloro-3-trifluoromethylphenyl)ureido)phenoxy)pyridine-2-carboxyllic acid methyamide-4-methylbenzenesulfonate

C21H16ClF3N4O3 (464.0863)


Sorafenib (rINN), marketed as Nexavar by Bayer, is a drug approved for the treatment of advanced renal cell carcinoma (primary kidney cancer). It has also received Fast Track designation by the FDA for the treatment of advanced hepatocellular carcinoma (primary liver cancer), and has since performed well in Phase III trials. Sorafenib is a small molecular inhibitor of Raf kinase, PDGF (platelet-derived growth factor), VEGF receptor 2 & 3 kinases and c Kit the receptor for Stem cell factor. A growing number of drugs target most of these pathways. The originality of Sorafenib lays in its simultaneous targeting of the Raf/Mek/Erk pathway. C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01E - Protein kinase inhibitors C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C61074 - Serine/Threonine Kinase Inhibitor C274 - Antineoplastic Agent > C1742 - Angiogenesis Inhibitor > C93259 - VEGFR Tyrosine Kinase Inhibitor C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C163953 - VEGFR-targeting Agent C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C164037 - PDGFR-targeting Agent C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C1967 - Tyrosine Kinase Inhibitor C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C2336 - Raf Kinase Inhibitor COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor D004791 - Enzyme Inhibitors > D047428 - Protein Kinase Inhibitors D000970 - Antineoplastic Agents Corona-virus Coronavirus SARS-CoV-2 COVID-19 SARS-CoV COVID19 SARS2 SARS Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].

   

Sorafenib

Sorafenib

C21H16ClF3N4O3 (464.0863)


C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor L - Antineoplastic and immunomodulating agents > L01 - Antineoplastic agents > L01E - Protein kinase inhibitors C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C61074 - Serine/Threonine Kinase Inhibitor C274 - Antineoplastic Agent > C1742 - Angiogenesis Inhibitor > C93259 - VEGFR Tyrosine Kinase Inhibitor C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C163953 - VEGFR-targeting Agent C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C164037 - PDGFR-targeting Agent C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C1967 - Tyrosine Kinase Inhibitor C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C2336 - Raf Kinase Inhibitor COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor D004791 - Enzyme Inhibitors > D047428 - Protein Kinase Inhibitors D000970 - Antineoplastic Agents Corona-virus Coronavirus SARS-CoV-2 COVID-19 SARS-CoV COVID19 SARS2 SARS Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].